{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,6]],"date-time":"2026-03-06T00:12:49Z","timestamp":1772755969606,"version":"3.50.1"},"reference-count":72,"publisher":"MDPI AG","issue":"2","license":[{"start":{"date-parts":[[2025,2,1]],"date-time":"2025-02-01T00:00:00Z","timestamp":1738368000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"National Institutes of Health","award":["GM134102"],"award-info":[{"award-number":["GM134102"]}]},{"name":"National Institutes of Health","award":["CHE-1659775"],"award-info":[{"award-number":["CHE-1659775"]}]},{"DOI":"10.13039\/100000001","name":"National Science Foundation","doi-asserted-by":"publisher","award":["GM134102"],"award-info":[{"award-number":["GM134102"]}],"id":[{"id":"10.13039\/100000001","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100000001","name":"National Science Foundation","doi-asserted-by":"publisher","award":["CHE-1659775"],"award-info":[{"award-number":["CHE-1659775"]}],"id":[{"id":"10.13039\/100000001","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Biomolecules"],"abstract":"<jats:p>Ghrelin is a 28 amino acid peptide hormone that impacts a wide range of biological processes, including appetite regulation, glucose metabolism, growth hormone regulation, and cognitive function. To bind and activate its cognate receptor, ghrelin must be acylated on a serine residue in a post-translational modification performed by ghrelin O-acyltransferase (GOAT). GOAT is a membrane-bound O-acyltransferase (MBOAT) responsible for the catalysis of the addition of an octanoyl fatty acid to the third serine of desacyl ghrelin. Beyond its canonical role for ghrelin maturation in endocrine cells within the stomach, GOAT was recently reported to be overexpressed in prostate cancer (PCa) cells and detected at increased levels in the serum and urine of PCa patients. This suggests GOAT can serve as a potential route for the detection and therapeutic targeting of PCa and other diseases that exhibit GOAT overexpression. Building upon a ghrelin mimetic peptide with nanomolar affinity for GOAT, we developed an antibody-conjugate-inspired system for customizable ligand-conjugate (LC) synthesis allowing for the attachment of a wide range of cargoes. The developed synthetic scheme allows for the easy synthesis of the desired LCs and demonstrates that our ligand system tolerates an extensive palette of cargoes while maintaining nanomolar affinity against GOAT.<\/jats:p>","DOI":"10.3390\/biom15020204","type":"journal-article","created":{"date-parts":[[2025,2,3]],"date-time":"2025-02-03T05:36:32Z","timestamp":1738560992000},"page":"204","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":1,"title":["A Modular Customizable Ligand-Conjugate (LC) System Targeting Ghrelin O-Acyltransferase"],"prefix":"10.3390","volume":"15","author":[{"ORCID":"https:\/\/orcid.org\/0009-0009-6224-7301","authenticated-orcid":false,"given":"Amber L.","family":"Ford","sequence":"first","affiliation":[{"name":"Department of Chemistry, Syracuse University, Syracuse, NY 13244, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Caine W.","family":"Taft","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Syracuse University, Syracuse, NY 13244, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Andrea M.","family":"Sprague-Getsy","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Syracuse University, Syracuse, NY 13244, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0009-0007-4065-5932","authenticated-orcid":false,"given":"Gracie C.","family":"Carlson","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Syracuse University, Syracuse, NY 13244, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4441-7188","authenticated-orcid":false,"given":"Nilamber A.","family":"Mate","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Syracuse University, Syracuse, NY 13244, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2765-7235","authenticated-orcid":false,"given":"Michelle A.","family":"Sieburg","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Syracuse University, Syracuse, NY 13244, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9518-2393","authenticated-orcid":false,"given":"John D.","family":"Chisholm","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Syracuse University, Syracuse, NY 13244, USA"},{"name":"BioInspired Syracuse, Syracuse University, Syracuse, NY 13244, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0444-1017","authenticated-orcid":false,"given":"James L.","family":"Hougland","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Syracuse University, Syracuse, NY 13244, USA"},{"name":"BioInspired Syracuse, Syracuse University, Syracuse, NY 13244, USA"},{"name":"Department of Biology, Syracuse University, Syracuse, NY 13244, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2025,2,1]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"656","DOI":"10.1038\/45230","article-title":"Ghrelin Is a Growth-Hormone-Releasing Acylated Peptide from Stomach","volume":"402","author":"Kojima","year":"1999","journal-title":"Nature"},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"649","DOI":"10.1016\/S0896-6273(03)00063-1","article-title":"The Distribution and Mechanism of Action of Ghrelin in the CNS Demonstrates a Novel Hypothalamic Circuit Regulating Energy Homeostasis","volume":"37","author":"Cowley","year":"2003","journal-title":"Neuron"},{"key":"ref_3","first-page":"E297","article-title":"Plasma ghrelin levels and hunger scores in humans initiating meals voluntarily without time- and food-related cues","volume":"287","author":"Cummings","year":"2004","journal-title":"Am. 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